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5Tr1 Aptamer-Pegylated Liposomal Doxorubicin Enhances Cellular Uptake and Suppresses Tumour Growth by Targeting Muc1 on the Surface of Cancer Cells Publisher Pubmed



Moosavian SA1 ; Abnous K2 ; Akhtari J3 ; Arabi L1 ; Gholamzade Dewin A4 ; Jafari M1
Authors
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Authors Affiliations
  1. 1. Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran
  2. 2. Pharmaceutical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran
  3. 3. Immunogenetics Research Center, Department of Medical Nanotechnology, School of Advanced Technologies in Medicine, Mazandaran University of Medical Sciences, Sari, Iran
  4. 4. Department of Pharmaceutical Science, Faculty of Pharmacy, Mashhad University of Medical Science, Mashhad, Iran

Source: Artificial Cells# Nanomedicine and Biotechnology Published:2018


Abstract

Employing targeting ligands with high affinity to tumour receptors is an important strategy to increase treatment efficacy. The use of aptamers as targeting agent is increasingly prevalent in drug delivery systems. Mucin1 (MUC1) is a glycoprotein that is over-expressed on the surface of several cancer cells and plays an important role in metastasis and invasion. 5TR1-aptamer is a DNA aptamer, which targets MUC1 receptors. The present study investigated the anti-tumour activity and therapeutic effectiveness of 5TR1-aptamer-PEGylated liposomal doxorubicin (PLD) delivery system in C26 tumour-bearing mice. The in vitro experiments demonstrated enhanced cytotoxicity and cellular uptake of PLD at the presence of 5TR1 aptamer into MUC1 + C26 cell line. Biodistribution study indicated that aptamer conjugation increased tumour accumulation of PLDs. Pharmacokinetic analysis showed despite higher clearance rate, selective delivery of doxorubicin to tumour tissue was increased in the 5TR1-Doxil group. In C26-bearing tumour mice, treatment with 5TR1-Doxil exhibited significant deceleration in tumour growth and enhanced survival. The results suggested that 5TR1 aptamer is promising ligand for active targeting which improves therapeutic efficiency of PLD in cancer therapy. © 2017, © 2017 Informa UK Limited, trading as Taylor & Francis Group.
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